PHA 767491 hydrochloride
Chemical Name: 1,5,6,7-Tetrahydro-2-(4-pyridinyl)-4H-pyrrolo[3,2-c]pyridin-4-one hydrochloride
Biological ActivityPHA 767491 hydrochloride is an ATP-competitive cyclin-dependent kinase (cdk) inhibitor (reported IC50 values are 0.034 - 0.75, 0.24 - 1.2, 0.25 - 1.1 and 0.46 - 1 μM for cdk9, cdk2, cdk1 and cdk5, respectively). Also inhibits mitogen-activated protein kinase-activated protein kinase-2 (MK2; IC50 = 171 nM). Prevents initiation of DNA replication. Inhibits cell proliferation in a variety of human cell lines and induces apoptosis in a p53-independent manner in vivo.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Pyrrolopyridine inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2).
Anderson et al.
Stopping replication, at the beginning.
Nature Chem.Biol., 2008;4:331
A cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumour activity.
Montagnoli et al.
Nature Chem.Biol., 2008;4:357
How selective are pharmacological inhibitors of cell-cycle-regulating cyclin-dependent kinases?
Jorda et al.
Citations for PHA 767491 hydrochloride
The citations listed below are publications that use Tocris products. Selected citations for PHA 767491 hydrochloride include:
5 Citations: Showing 1 - 5
DDK dependent regulation of TOP2A at centromeres revealed by a chemical genetics approach.
Authors: Wu Et al.
Nucleic Acids Res 2016;44:8786
Mammalian FMRP S499 Is Phosphorylated by CK2 and Promotes Secondary Phosphorylation of FMRP.
Authors: Bartley Et al.
A high through-put screen for small molecules modulating MCM2 phosphorylation identifies Ryuvidine as an inducer of the DNA damage response.
Authors: FitzGerald Et al.
PLoS One 2014;9:e98891
CDC7 inhibition blocks pathological TDP-43 phosphorylation and neurodegeneration.
Authors: Liachko Et al.
Ann Neurol 2013;74:39
Geminin overexpression prevents the completion of topoisomerase IIα chromosome decatenation, leading to aneuploidy in human mammary epithelial cells.
Authors: Gardner Et al.
Breast Cancer Res 2011;13:R53
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